CAS: 1141397-80-9; (R)-1-((2R,4R,5R)-3,3-Difluoro-4-Hydroxy-5-(Hydroxymethyl)Tetrahydrofuran-2-yl)-4-Hydroxytetrahydropyrimidin-2(1H)-One

该化合物是一种核素类比,主要作为细胞碘脱氨酶的抑制剂,一种降解细胞碘及其类似物的酶,这种特性提高了某些乳胶化剂的生物利用率和功效,特别是在治疗癌症方面;Cedazuridine经常与其他药物结合使用,以提高其治疗效果,同时减少毒性;该化合物通常以口头方式施用,并因其在加强核素类比的药理基因学方面的作用而著称,允许较低剂量,并可能减少副作用;其行动机制包括防止将细胞碘转换为碘,从而增加人体中活跃的核素类比水平;Cedazuridine在各种临床环境中,特别是皮肤恶性病方面受到研究,并继续是癌症研究中可能改善治疗结果的一个领域.

结构式图片

欧盟法规

C&L通报

上下游产品

2'-Deoxy-2',2'-Difluoro-5,6-Dihydrouridine 1141397-77-4

合成工艺路线路线简述

  • 合成目标产物 (R)-1-((2R, 4R, Sr)-3,3-Difluoro-4-Hydroxy (Hydroxymethyl) Tetrahydrofuran-2-yl)-4-Hydroxytetrahydropyrimidin-2(1H)-One 主要起始原料 Uridine, 2'-Deoxy-2',2'-Difluoro-3,4,5,6-Tetrahydro-
  • (文献来源)合成步骤主要原料 Uridine, 2'-Deoxy-2',2'-Difluoro-3,4,5,6-Tetrahydro-
[(2R,3R,5R)-3-Benzoyloxy-5-(2,4-Dioxo-1,3-Diazinan-1-yl)-4,4-Difluorooxolan-2-Yl]Methyl Benzoate置于cerium(III) Chloride Heptahydrate,氨,1,8-二氮杂双环[5.4.0]十一碳-7-烯体系中,用 甲醇,乙醇,二氯甲烷,水,乙腈 用作溶剂,化学反应 119.08H,反应生成西达尿苷
参考文献: Synthetic Route To 2'-Deoxy-2',2'-Difluorotetrahydrouridines[fr] Voie De Synthèse Pour 2'-Désoxy-2',2'-Difluorotétrahydrouridines
标题: Synthetic Route To 2'-Deoxy-2',2'-Difluorotetrahydrouridines[fr] Voie De Synthèse Pour 2'-Désoxy-2',2'-Difluorotétrahydrouridines
摘要:本发明涉及合成2'-脱氧-2',2'-二氟四氢尿苷化合物的方法和中间体.

海关参考信息

专利信息


专利号:US-10954178-B1
优先权日:2020-08-28
标题 :Synthesis of haloindenes
发明人:WNUK STANISLAW F; HOWLADER MD ABU HASAN
权利人:WNUK STANISLAW F; HOWLADER MD ABU HASAN; THE FLORIDA INTERNATIONAL UNIV BOARD OF TRUSTEES
摘要:The subject invention provides an expedited synthesis of 5, 6, and 7-iodoindenes from the corresponding aminoindan-1-ones in more than 70% yield, employing readily available precursors and reagents. A three-step sequence involves diazotization-iodination of aminoindan-1-one followed by reduction and dehydration. The method has a general character and can be extended for the preparation of various 4-, 5-, 6- or 7-haloindenes using different halogen sources for diazotization-halogenation reaction.

专利号:US-11873305-B2
优先权日:2020-06-30
标题 :Processes for synthesis of substituted indole intermediates for the synthesis of serd compounds
发明人:ZHANG HAIMING; XU JIE; WUITSCHIK GEORG; ANGELAUD REMY; HEROLD SEBASTIAN; STUTZ ALFRED; BRUETSCH TOBIAS; BURKHARD JOHANNES
权利人:GENENTECH INC; HOFFMANN LA ROCHE
摘要:Provided herein are processes for the preparation of indolyl intermediates using Wenker Synthesis for the total synthesis of SERD compounds useful in the treatment of cancer.

专利号:US-10889599-B2
优先权日:2018-02-27
标 题:1,1-diborylalkyl-1-metal compounds, preparation method thereof, and their applications toward synthesis of 1,1-diboronate ester compounds
发明人:CHO SEUNG HWAN; LEE YEOSAN
权利人:POSTECH ACAD IND FOUND
摘要:The present invention relates to a 1,1-diborylalkyl-1-metal compound including one metal group together with two identical boron groups at the sp3 carbon center, and its use. Specifically, the present invention relates to development of novel organic reactions, synthesis of functional molecules, and synthesis of new drugs by applying the novel 1,1-diboryl-1-metal substituted alkyl compounds to various molecular libraries which could not be synthesized by conventional methodologies.

专利号:US-9809566-B2
优先权日:2012-09-06
标题:Organocatalytic process for asymmetric synthesis of decanolides
发明人:RAWAT VARUN; DEY SOUMEN; SHELKE ANIL MARUTI; SURYAVANSHI GURUNATH MALLAPPA; SUDALAI ARUMUGAM
权利人:COUNCIL SCIENT IND RES
摘要:The present invention discloses organocatalytic process for asymmetric synthesis of highly enantioselective decanolide compounds in high yield with >99% ee. Further, the present invention disclose cost effective, improved organocatalytic process for asymmetric synthesis of highly enantioselective decanolides compounds from non-chiral, cheap, easily available raw materials.

专利号:US-7173059-B2
优先权日:2003-05-08
标题:Intermediates useful in the synthesis of HIV-protease inhibitors and methods for preparing the same
发明人:ALBIZATI KIM FRANCIS; BABU SRINIVASAN
权利人:AGOURON PHARMA
摘要:Optically active 3-amino-butene and 1,2-dihydroxy-3-amino-butane intermediate compounds, useful in the synthesis of HIV-protease inhibitors and methods of preparing these intermediate compounds are disclosed.

专利号:US-11325912-B2
优先权日:2019-05-09
标题 :Regio-selective synthesis of imidazo[1,2-a]pyrimidines
发明人:CLAGG KYLE BRADLEY PASCUAL; WHITE NICHOLAS ANDREW; ZHANG HAIMING; GOSSELIN FRANCIS; NACK WILLIAM; O'SHEA PAUL D
权利人:GENENTECH INC
摘要:A method of regio-selectively synthesizing an imidazo-pyrimidine compound of formulae (XXa) or (XXb)comprising a step of coupling a first compound of formula XX-P1a or XX-P1b with a second compound of formula XX-P2This annulation reaction between β-ethoxy acrylamides and phosphorylated aminoimidazoles to furnish imidazo[1,2-a]pyrimidin-amines relies on steering effects from endocyclic and exocyclic phosphorylated aminoimidazoles. The reaction furnishes either 2-amino or 4-amino constitutional isomers of imidazo[1,2-a]pyrimidines with good yields and ranges of 90:10-99:1 regio-selectivity. The reaction is useful in the synthesis of various tracer molecules used in the study of neurological conditions such as where R3 and R4 together with the imidazole ring atoms to which they are bonded form a phenyl ring and the products are substituted benzimidazopyrimidines. The reaction can be generalized to form imidazo[1,2-a]pyrimidines substituted at either of their 2- and 4-positions by alkoxy or thioalkyl groups.
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合成参考文献


摘要:Ferraris D, Duvall B, Delahanty G, Mistry B, Alt J, Rojas C, Rowbottom C, Sanders K, Schuck E, Huang KC, Redkar S, Slusher BB, Tsukamoto T: Design, synthesis, and pharmacological evaluation of fluorinated tetrahydrouridine derivatives as inhibitors of cytidine deaminase. J Med Chem. 2014 Mar 27;57(6):2582-8. doi: 10.1021/jm401856k. Epub 2014 Feb 24.
摘要:Kleemann A., Kutscher B., Reichert D., Bossart M., Pharmaceutical Substances, Thieme [Online], Stuttgart, (2025).
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